Expanding the Scope of Human DNA Polymerase λ and ß Inhibitors

Zitieren

Dateien zu dieser Ressource

Dateien Größe Format Anzeige

Zu diesem Dokument gibt es keine Dateien.

STRITTMATTER, Tobias, Anette BROCKMANN, Moritz POTT, Annika HANTUSCH, Thomas BRUNNER, Andreas MARX, 2014. Expanding the Scope of Human DNA Polymerase λ and ß Inhibitors. In: ACS Chemical Biology. 9(1), pp. 282-290. ISSN 1554-8929. eISSN 1554-8937

@article{Strittmatter2014-01-17Expan-25889, title={Expanding the Scope of Human DNA Polymerase λ and ß Inhibitors}, year={2014}, doi={10.1021/cb4007562}, number={1}, volume={9}, issn={1554-8929}, journal={ACS Chemical Biology}, pages={282--290}, author={Strittmatter, Tobias and Brockmann, Anette and Pott, Moritz and Hantusch, Annika and Brunner, Thomas and Marx, Andreas} }

<rdf:RDF xmlns:rdf="http://www.w3.org/1999/02/22-rdf-syntax-ns#" xmlns:bibo="http://purl.org/ontology/bibo/" xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:dcterms="http://purl.org/dc/terms/" xmlns:xsd="http://www.w3.org/2001/XMLSchema#" > <rdf:Description rdf:about="https://kops.uni-konstanz.de/rdf/resource/123456789/25889"> <dc:creator>Hantusch, Annika</dc:creator> <dcterms:rights rdf:resource="http://nbn-resolving.org/urn:nbn:de:bsz:352-20140905103605204-4002607-1"/> <dc:creator>Pott, Moritz</dc:creator> <bibo:uri rdf:resource="http://kops.uni-konstanz.de/handle/123456789/25889"/> <dc:creator>Marx, Andreas</dc:creator> <dc:contributor>Marx, Andreas</dc:contributor> <dc:contributor>Hantusch, Annika</dc:contributor> <dc:language>eng</dc:language> <dc:contributor>Brockmann, Anette</dc:contributor> <dc:contributor>Brunner, Thomas</dc:contributor> <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2014-01-22T10:07:30Z</dcterms:available> <dcterms:title>Expanding the Scope of Human DNA Polymerase λ and ß Inhibitors</dcterms:title> <dc:contributor>Pott, Moritz</dc:contributor> <dc:rights>deposit-license</dc:rights> <dcterms:bibliographicCitation>ACS chemical biology ; 9 (2014), 1. - S. 282-290</dcterms:bibliographicCitation> <dc:creator>Brockmann, Anette</dc:creator> <dcterms:issued>2014-01-17</dcterms:issued> <dc:creator>Brunner, Thomas</dc:creator> <dcterms:abstract xml:lang="eng">The exact biological functions of individual DNA polymerases still await clarification, and therefore appropriate reagents to probe their respective functions are required. In the present study, we report the development of a highly potent series of human DNA polymerase λ and β (pol λ and β) inhibitors based on the rhodanine scaffold. Both enzymes are involved in DNA repair and are thus considered as future drug targets. We expanded the chemical diversity of the small-molecule inhibitors arising from a high content screening and designed and synthesized 30 novel analogues. By biochemical evaluation, we discovered 23 highly active compounds against pol λ. Importantly, 10 of these small-molecules selectively inhibited pol λ and not the homologous pol β. We discovered 14 small-molecules that target pol β and found out that they are more potent than known inhibitors. We also investigated whether the discovered compounds sensitize cancer cells toward DNA-damaging reagents. Thus, we cotreated human colorectal cancer cells (Caco-2) with the small-molecule inhibitors and hydrogen peroxide or the approved drug temozolomide. Interestingly, the tested compounds sensitized Caco-2 cells to both genotoxic agents in a DNA repair pathway-dependent manner.</dcterms:abstract> <dc:contributor>Strittmatter, Tobias</dc:contributor> <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2014-01-22T10:07:30Z</dc:date> <dc:creator>Strittmatter, Tobias</dc:creator> </rdf:Description> </rdf:RDF>

Das Dokument erscheint in:

KOPS Suche


Stöbern

Mein Benutzerkonto